Ifenprodil-like NMDA receptor negative allosteric modulator based on the biphenyl scaffold has been identified using virtual screening. Docking approach demonstrated that the modulator maintains some characteristic interactions with protein similar to ifenprodil. Electrophysiological and radioligand investigations demonstrated the concentration-dependent NMDA/Gly-induced currents inhibition with IC50 = 5 μM and significant displacement of [H3]ifenprodil with EC50 = 30 μM, respectively.
- biphenyl scaffold
- electrophysiological investigations
- negative allosteric modulator
- NMDA receptors